This invention relates to the use of trimoprostil and its derivatives in the treatment of glaucoma and ocular hypertension. These compounds have the following formula: ##STR1## wherein R.sup.1 is hydrogen, a cationic salt moiety, a pharmaceutically acceptable amine moiety or a pharmaceutically acceptable ester moiety derived from the corresponding alcohol; and R.sup.2 is hydrogen or a pharmaceutically acceptable ester moiety derived from the corresponding carboxylic acid.
Natural prostaglandins are known to lower intraocular pressure (IOP) after topical ocular instillation, but can cause an inflammatory response. Many synthetic prostaglandins have been observed to lower intraocular pressure, but most such compounds also produce the described inflammatory response. Unexpectedly, trimoprostil has been found to cause a lowering of the IOP at a dose that does not create an inflammatory response, that is, cause breakdown of the blood-aqueous barrier as evidenced by a lack of increase in aqueous humor protein concentration. These observations have been made in rabbits, a model designed to be validly predictive of the human response. Trimoprostil is a known compound with utility alleged in the systemic treatment for gastrointestinal tract ulcers.